Structural basis for androgen receptor agonists and antagonists: Interaction of SPEED 98-listed chemicals and related compounds with the androgen receptor based on an in vitro reporter gene assay and 3D-QSAR

2006 ◽  
Vol 14 (21) ◽  
pp. 7160-7174 ◽  
Author(s):  
Hiroto Tamura ◽  
Yoichi Ishimoto ◽  
Tomoko Fujikawa ◽  
Hiroaki Aoyama ◽  
Hiromichi Yoshikawa ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Reporter Gene ◽  
3D Qsar ◽  
Reporter Gene Assay ◽  
Structural Basis ◽  
Receptor Agonists ◽  
Gene Assay ◽  
Related Compounds ◽  
Receptor Agonists And Antagonists

scholarly journals In vitro bioanalytical assessment of toxicity of wetland samples from Spanish Mediterranean coastline

2021 ◽  
Vol 33 (1) ◽  
Author(s):  
Alberto Celma ◽  
Geeta Mandava ◽  
Agneta Oskarsson ◽  
Juan Vicente Sancho ◽  
Lubertus Bijlsma ◽  
...  
Keyword(s):  
Water Quality ◽  
Reporter Gene ◽  
Biological Activities ◽  
Reporter Gene Assay ◽  
Water Bodies ◽  
Good Tool ◽  
Adverse Health Effects ◽  
Aryl Hydrocarbon ◽  
Gene Assay

Abstract Background Fresh water bodies represent less than 1% of overall amount of water on earth and ensuring their quality and sustainability is pivotal. Although several campaigns have been performed to monitor the occurrence of micropollutants by means of chemical analysis, this might not cover the whole set of chemicals present in the sample nor the potential toxic effects of mixtures of natural and anthropogenic chemicals. In this sense, by selecting relevant toxicity endpoints when performing in vitro bioanalysis, effect-based methodologies can be of help to perform a comprehensive assessment of water quality and reveal biological activities relevant to adverse health effects. However, no prior bioanalytical study was performed in wetland water samples from the Spanish Mediterranean coastline. Methods Eleven samples from relevant water bodies from the Spanish Mediterranean coastline were collected to monitor water quality on 8 toxicity endpoints. Aryl hydrocarbon receptor (AhR), androgenicity (AR+ and AR−), estrogenicity (ER+ and ER−), oxidative stress response (Nrf2) and vitamin D receptor (VDR+ and VDR−) reporter gene assays were evaluated. Results AhR was the reporter gene assay showing a more frequent response over the set of samples (activated by 9 out of 11 samples), with TCDD-eq in the range 7.7–22.2 pM. For AR, ER and VDR assays sporadic activations were observed. Moreover, no activity was observed on the Nrf2 reporter gene assay. Wastewater and street runaway streams from Valencia could be responsible for enhanced activities in one of the water inputs in the Natural Park ‘L’Albufera’. Conclusions Water quality of relevant wetlands from the Spanish Mediterranean coastline has been evaluated. The utilization of a panel of 5 different bioassays to cover for different toxicity endpoints has demonstrated to be a good tool to assess water quality.

Evaluation of estrogenic activities of pesticides using an in vitro reporter gene assay

2005 ◽  
Vol 15 (4) ◽  
pp. 271-280 ◽  
Author(s):  
Mihoko Kojima ◽  
Kenji Fukunaga * ◽  
Mari Sasaki ◽  
Masafumi Nakamura ◽  
Motohiro Tsuji ◽  
...  
Keyword(s):  
Reporter Gene ◽  
Reporter Gene Assay ◽  
Gene Assay

Evaluation of Estrogenic Activity of Wastewater: Comparison Among In Vitro ERα Reporter Gene Assay, In Vivo Vitellogenin Induction, and Chemical Analysis

2015 ◽  
Vol 49 (10) ◽  
pp. 6319-6326 ◽  
Author(s):  
Masaru Ihara ◽  
Tomokazu Kitamura ◽  
Vimal Kumar ◽  
Chang-Beom Park ◽  
Mariko O. Ihara ◽  
...  
Keyword(s):  
Chemical Analysis ◽  
Reporter Gene ◽  
Estrogenic Activity ◽  
Reporter Gene Assay ◽  
Gene Assay

Downscaling procedures reduce chemical use in androgen receptor reporter gene assay

2016 ◽  
Vol 571 ◽  
pp. 826-833 ◽  
Author(s):  
Carolina Di Paolo ◽  
Kristina Kirchner ◽  
Fabian Gerhard Peter Balk ◽  
Matthias Muschket ◽  
Werner Brack ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Reporter Gene ◽  
Reporter Gene Assay ◽  
Gene Assay

In vitro Estrogenicity of Resin Composites

2004 ◽  
Vol 83 (3) ◽  
pp. 222-226 ◽  
Author(s):  
H. Wada ◽  
H. Tarumi ◽  
S. Imazato ◽  
M. Narimatsu ◽  
S. Ebisu
Keyword(s):  
Bisphenol A ◽  
Reporter Gene ◽  
Estrogenic Activity ◽  
Reporter Gene Assay ◽  
Resin Composites ◽  
Minimum Concentration ◽  
Tert Butyl ◽  
Gene Assay

Previously, we have reported that sealants incorporating bisphenol A dimethacrylate showed estrogenicity by a reporter gene assay. This study tested the hypothesis that commercial composites, which contain various monomers and additives, exhibit estrogenic activity in vitro. The estrogenic activities of eluates obtained from 24 composites and 18 chemicals identified from the composites tested were examined with the use of the reporter gene assay. Among the 24 composites, 6 products were estrogenic, and among the 18 constituents, 1 photostabilizer, 2-hydroxy-4-methoxy-benzophenone (HMBP), 1 photoinitiator, 2,2-dimethoxy-2-phenyl-acetophenone (DMPA), and 1 inhibitor, 2,6-di- tert-butyl- p-cresol (BHT) had significant estrogenic activity. The concentration of HMBP in 4 estrogenic eluates was greater than the minimum concentration required for estrogenicity, and DMPA was found at a higher level than the minimum estrogenic concentration in the remaining 2 estrogenic specimens. These results suggest that the observed estrogenic activity of 6 composites is associated with the elution of either HMBP or DMPA.

An in Vitro Reporter Gene Assay Method Incorporating Metabolic Activation with Human and Rat S9 or Liver Microsomes

2001 ◽  
Vol 280 (1) ◽  
pp. 85-91 ◽  
Author(s):  
Kayo Sumida ◽  
Norihisa Ooe ◽  
Hirohisa Nagahori ◽  
Koichi Saito ◽  
Naohiko Isobe ◽  
...  
Keyword(s):  
Reporter Gene ◽  
Liver Microsomes ◽  
Metabolic Activation ◽  
Reporter Gene Assay ◽  
Assay Method ◽  
Gene Assay

In vitro regulation of reporter gene transcription by the androgen receptor AF1 domain

2004 ◽  
Vol 32 (6) ◽  
pp. 1103-1106 ◽  
Author(s):  
M.A. Choudhry ◽  
I.J. McEwan
Keyword(s):  
Gene Expression ◽  
Androgen Receptor ◽  
Reporter Gene ◽  
Protein Interactions ◽  
Transcription Initiation ◽  
Muscular Atrophy ◽  
Activation Function ◽  
Regulation Of Transcription ◽  
Gene Assay

The androgen receptor (AR) is a ligand-activated transcription factor that regulates gene expression in response to the steroids testosterone and dihydrotestosterone. AR-dependent gene expression is likely to play an important role in a number of receptor-associated disorders, such as prostate cancer, spinal bulbar muscular atrophy, male type baldness and hirsutism. The AR contains two transactivation domains, termed AF1 (activation function 1) located in the N-terminus and AF2 (activation function 2) in the C-terminal ligand-binding domain. AF2 exhibits weak transcriptional activity, whereas AF1 is a strong regulator of transcription. Transcriptional regulation by AF1 is thought to be modulated by a number of proteins that interact with this region, and by post-translational modifications. Our focus is on the N-terminal-interacting proteins and their regulation of transcription via interaction with the receptor. To better understand the mechanism of AR-AF1 action, we have reconstituted AR activity in HeLa nuclear extracts using a unique dual reporter gene assay. Multiple LexA-binding sites in the promoter allow transcription to be driven by a recombinant AR-AF1–Lex fusion protein. The findings from initial experiments suggest an increase in transcription initiation and elongation rates by AR-AF1–Lex. The role of protein–protein interactions involving co-activators and basal transcription factors and AR-AF1 activity are discussed.

Establishment of an in vitro reporter gene assay for developmental cardiac toxicity

2001 ◽  
Vol 15 (3) ◽  
pp. 215-223 ◽  
Author(s):  
S Bremer ◽  
A.P Worth ◽  
M Paparella ◽  
K Bigot ◽  
E Kolossov ◽  
...  
Keyword(s):  
Reporter Gene ◽  
Cardiac Toxicity ◽  
Reporter Gene Assay ◽  
Gene Assay
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